Triazolopyrimidinones as γ-secretase modulators: structure–activity relationship, modulator profile, and in vivo profiling

Abstract

The structure–activity relationship for a series of potent γ-secretase modulators based on the 6,7-dihydro-4H-[1,2,4]triazolo[1,5-a]pyrimidin-5-one scaffold is described. Furthermore, we report details regarding the modulator profile on Aβ processing, as well as in vivo efficacy, for the optimized compounds.